Solubility enhancement of hydrophobic compounds by cosolvents: Role of solute hydrophobicity on the solubilization effect

Miyako, Yasuhiro; Khalef, Nawel; Matsuzaki, Katsumi; Pinal, Rodolfo

doi:10.1016/j.ijpharm.2010.03.059

Cited by 78 publications

(26 citation statements)

References 21 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…A number of formulation approaches have been used to improve water solubility of hydrophobic drugs. These include cyclodextrin complexation, co-solvent systems, salt-forming techniques, prodrug formation, particle size reduction and self-microemulsifying drug delivery systems (SMEDDS) (Brewster and Loftsson, 2007;Fleisher et al, 1996;Hintzen et al, 2014;McConville and Friend, 2013;Millard et al, 2002;Miyako et al, 2010;Serajuddin, 2007).…”

Section: Introductionmentioning

confidence: 99%

Preparation and characterisation of Kolliphor® P 188 and P 237 solid dispersion oral tablets containing the poorly water soluble drug disulfiram

Ramadhani

Shabir

McConville

2014

International Journal of Pharmaceutics

View full text Add to dashboard Cite

Section: Introductionmentioning

confidence: 99%

Preparation and characterisation of Kolliphor® P 188 and P 237 solid dispersion oral tablets containing the poorly water soluble drug disulfiram

Ramadhani

Shabir

McConville

2014

International Journal of Pharmaceutics

View full text Add to dashboard Cite

“…According to the assumption that the effect of solute‐solvent interactions in the mixture as the (volume fraction) weighted average of the interactions in pure solvents, Yalkowsky and co‐workers introduced the L‐L model, which can be expressed in the form

ln x_{3} = x_{1} ln X_{1} + x_{2} ln X_{2} = ln X_{2} + σ x_{1},

where x 1 and x 2 are the mole fractions of cosolvent and water in binary solvent mixtures and X 1 , X 2 , and x 3 refers to the mole fraction solubility of solute in pure cosolvent, water, and binary solvent mixtures, respectively. σ =ln( X 1 / X 2 ) is the solubilization power of the cosolvent . From the expression of Equation , it can be found a straight line for ln x 3 as a function of cosolvent fraction, corresponding to the monotonic increasing as the cosolvent fraction increased…”

Section: Introductionmentioning

confidence: 99%

“…There are several models, namely, the log‐linear (L‐L) model, the modified Wilson (MW) model, mixture response surface model, and the Williams–Amidon (WA) model, have been published in literatures to correlate the solubility of solute (s) in cosolvent + water mixtures. A deep reviewing of these models has been performed by Jouyban in “Handbook of Solubility of Pharmaceuticals.”…”

Section: Introductionmentioning

confidence: 99%

Estimation of the solubility with cosolvent composition by combinated of the Williams–Amidon model with quasi virial coefficient

Wang

Zhang

2019

Asia-Pacific J Chem Eng

View full text Add to dashboard Cite

TABLE 1 Accuracy of different cosolvency models for luteolin 21 at 313.15 K Models R 2 RMSD Log-linear model 0.913 1.53 × 10 −1 Modified Wilson model 0.999 1.70 × 10 −2 Williams-Amidon model 0.996 3.06 × 10 −2 WA-QVC model 0.999 1.81 × 10 −3 Jouyban-Acree model 0.999 1.84 × 10 −3 RMSD, root-mean-square deviation.TABLE 2 Parameters of WA-QVC model for luteolin 21 at different temperatures T/K 273.15 283.15 293.15 303.15 313.15 323.15 B 1 4.80 × 10 −7

show abstract

“…Various cosolvents used include different grades of polyethylene glycols like PEG 100, PEG 200, PEG 300, PEG 400, and PEG 600; propylene glycols; glycerol; diethylene glycol monoethyl ether; pyrrolidones; glycofurol; alcohol; Soluphor P; Pharmasolve; etc. (27)(28)(29). The primary concern of a cosolventbased approach is the precipitation of solubilized drug upon dilution with aqueous fluids.…”

Section: Conventional Approachesmentioning

confidence: 99%

Preclinical Formulations: Insight, Strategies, and Practical Considerations

et al. 2014

View full text Add to dashboard Cite

Abstract. A lot of resources and efforts have been directed to synthesizing potentially useful new chemical entities (NCEs) by pharmaceutical scientists globally. Detailed physicochemical characterization of NCEs in an industrial setup begins almost simultaneously with preclinical testing. Most NCEs possess poor water solubility posing bioavailability issues during initial preclinical screening, sometimes resulting in dropping out of an NCE with promising therapeutic activity. Selection of right formulation approach for an NCE, based on its physicochemical properties, can aid in improving its solubility-related absorption and bioavailability issues. The review focuses on preclinical formulations stressing upon different preclinical formulation strategies and deciphers the understanding of formulation approaches that could be employed. It also provides detailed information related to a vast pool of excipients available today, which is of immense help in designing preclinical formulations. Few examples mentioned, throw light on key aspects of preclinical formulation development. The review will serve as an important guide for selecting the right strategy to improve bioavailability of NCEs for academic as well as industrial formulation scientists.

show abstract

Solubility enhancement of hydrophobic compounds by cosolvents: Role of solute hydrophobicity on the solubilization effect

Cited by 78 publications

References 21 publications

Preparation and characterisation of Kolliphor® P 188 and P 237 solid dispersion oral tablets containing the poorly water soluble drug disulfiram

Preparation and characterisation of Kolliphor® P 188 and P 237 solid dispersion oral tablets containing the poorly water soluble drug disulfiram

Estimation of the solubility with cosolvent composition by combinated of the Williams–Amidon model with quasi virial coefficient

Preclinical Formulations: Insight, Strategies, and Practical Considerations

Contact Info

Product

Resources

About